Planta Medica, Table of Contents

Planta Med 2016; 82(16): 1425-1430
DOI: 10.1055/s-0042-112594

Biological and Pharmacological Activity

Original Papers

Georg Thieme Verlag KG Stuttgart · New York

Estrogenic Activity of Hyperforin in MCF-7 Human Breast Cancer Cells Transfected with Estrogen Receptor

Joseph Kwon^*

¹Korea Basic Science Institute, Daejeon, Republic of Korea

,

Kyung Seo Oh^*

²Department of Food Science and Technology and BK21 Plus Program, Chonnam National University, Gwangju, Republic of Korea

,

Se-Young Cho^*

²Department of Food Science and Technology and BK21 Plus Program, Chonnam National University, Gwangju, Republic of Korea

,

Mi Ae Bang^*

³Jeonnam Biofood Technology Center, Naju, Republic of Korea

,

Hwan Seon Kim

²Department of Food Science and Technology and BK21 Plus Program, Chonnam National University, Gwangju, Republic of Korea

,

Bipin Vaidya

²Department of Food Science and Technology and BK21 Plus Program, Chonnam National University, Gwangju, Republic of Korea

⁴Bioenergy Research Center, Chonnam National University, Gwangju, Republic of Korea

,

Duwoon Kim

²Department of Food Science and Technology and BK21 Plus Program, Chonnam National University, Gwangju, Republic of Korea

⁴Bioenergy Research Center, Chonnam National University, Gwangju, Republic of Korea

⁵Foodborne Virus Research Center, Chonnam National University, Gwangju, Republic of Korea

› Author Affiliations

Abstract

Hyperforin, a major active compound of St. Johnʼs wort extract, affects estrogenic activity. In this study, the compound evoked estrogen response element-dependent luciferase activity and cell proliferation in MCF-7 cells. Hyperforin-induced cell proliferation was significantly inhibited by the estrogen receptor antagonist ICI 182,780. These results suggested that hyperforin had estrogenic and cell proliferation activities, which were stimulated via the estrogen receptor. Compared to 17β-estradiol, hyperforin showed significantly lower estrogenic activity and cell proliferation. The mechanism underlying the estrogenic activity of hyperforin was unknown, therefore, in this study, for the first time, the expression and post-translational modification of proteins were determined and compared among control, 17β-estradiol-treated, and hyperforin-treated cells using proteomic techniques. A total of 453 proteins were identified, of which 282 proteins were significantly modulated in hyperforin-treated cells compared to 17β-estradiol-treated cells. Ingenuity pathway analysis also demonstrated that hyperforin treatment induced less cell proliferation than 17β-estradiol by downregulating estrogen receptor 1. Protein network analysis showed that cell proliferation was regulated mainly by cyclin D1 and extracellular signal-regulated kinases. In conclusion, although, hyperforin exhibited lower estrogenic activity than 17β-estradiol, the compound induced lower levels of cancer cell proliferation in vitro.

Key words

Key words

Clusiaceae - estrogenic activity - hyperforin - Hypericum perforatum - Proteomics - St. Johnʼs wort

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Supplementary Material

Supplementary Material

Supporting Information